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测量受体靶点覆盖率：一种用于评估未标记化合物结合和解离速率的放射性配体竞争结合方案。

Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds.

作者信息

Sykes David A, Dowling Mark R, Charlton Steven J

机构信息

Novartis Institutes for Biomedical Research, Horsham, West Sussex, United Kingdom.

出版信息

Curr Protoc Pharmacol. 2010 Sep;Chapter 9:Unit 9.14. doi: 10.1002/0471141755.ph0914s50.

DOI:10.1002/0471141755.ph0914s50
PMID:22294377
Abstract

The kinetics of the ligand-receptor interaction is an important feature in lead optimization for new drug candidates. The protocol described in this unit is a kinetic radioligand competition binding assay that makes possible the determination of both the association and dissociation rates of unlabeled receptor ligands.

摘要

配体-受体相互作用的动力学是新药候选物先导优化中的一个重要特征。本单元所述的实验方案是一种动力学放射性配体竞争结合测定法，它使测定未标记受体配体的结合和解离速率成为可能。

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